Search results for "Drug Inverse Agonism"

showing 2 items of 2 documents

A systematic review of inverse agonism at adrenoceptor subtypes

2020

As many, if not most, ligands at G protein-coupled receptor antagonists are inverse agonists, we systematically reviewed inverse agonism at the nine adrenoceptor subtypes. Except for β3-adrenoceptors, inverse agonism has been reported for each of the adrenoceptor subtypes, most often for β2-adrenoceptors, including endogenously expressed receptors in human tissues. As with other receptors, the detection and degree of inverse agonism depend on the cells and tissues under investigation, i.e., they are greatest when the model has a high intrinsic tone/constitutive activity for the response being studied. Accordingly, they may differ between parts of a tissue, for instance, atria vs. ventricles…

Cell typeDrug Inverse AgonismAdrenergic receptorDrug discoveryChemistryinverse agonismReviewpharmacology_toxicology570 Life sciencesBasal (phylogenetics)lcsh:Biology (General)Drug DevelopmentDrug developmentHumansInverse agonistAgonismReceptors Adrenergic beta-2Receptorlcsh:QH301-705.5adrenoceptorconstitutive activityNeuroscience570 Biowissenschaften
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Effects of the benzodiazepine inverse agonist FG7142 on the structure of anxiety-related behavior of male Wistar rats tested in hole board

2016

Little is known about the structural characteristics of the behavior of rats with enhanced anxiety level. To fill this gap, a study was undertaken where effects of an anxiogenic drug were examined on behavioral structure of rats tested in hole board.This study investigates effects of increased anxiety level on the structure of the behavior of rats tested in hole board METHODS: Different doses of FG7142 (1, 4, 8 mg/kg IP), a potent anxiety-inducing drug, were administered to three groups of male Wistar rats. A further group was administered saline. Experiments were recorded through a digital camera. Quantitative and multivariate approaches were applied.Percent distributions and durations sho…

MaleSettore M-PSI/01 - Psicologia Generalemedicine.medical_specialtyDrug Inverse Agonismmedicine.drug_classmedicine.medical_treatmentHead dipEnvironmentMotor ActivityAdjusted residualAnxietyWistar ratSettore BIO/09 - FisiologiaGABA Antagonists03 medical and health sciences0302 clinical medicineSniffingInternal medicineGrooming activitiesmedicineAnimalsInverse agonistCluster analysiRats WistarSalineEdge sniffPharmacologyBenzodiazepineBehavior AnimalReceptors GABA-AFG7142Rats030227 psychiatryEndocrinologyAnxiogenicExploratory BehaviorHole boardAnxietyTransition matricesmedicine.symptomCarrier ProteinsPsychology030217 neurology & neurosurgeryCarbolinesPsychopharmacology
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